JSH-150

SKU: orb1298895

Description

JSH-150 is a potent and highly selective inhibitor of CDK9 with an IC50 of 1 nM. This compound is a valuable research tool for investigating CDK9-dependent transcription in oncology and virology research, applicable in both cellular and biochemical assays.

Research Area

Cell Biology

Key Properties

• CAS Number: 2247481-21-4
• MW: 505.08
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₃₃ClN₆O₂S
• SMILES: COCCN[C@H]1CC[C@@H](CC1)Nc1cc(-c2csc(NCC3(CCOCC3)C#N)n2)c(Cl)cn1
• Target: CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.96 mM);DMSO:55 mg/mL (108.89 mM)

Bioactivity

• Target IC50:
  CDK9-CyclinT1:1 nM|CDK7-CyclinH-MNAT1:1.72 μM|CDK1-CyclinB:1.34 μM|CDK16-CyclinY:292 nM|CDK14-CyclinY:1.68 μM|CDK2-CyclinA:2.86 μM|CDK5-p25:4.64 μM
• In Vivo:
  In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of 40 could almost completely suppress the tumor progression. The high selectivity and good in vivo PK/PD profile suggested that 40 would be a good pharmacological tool to study CDK9-mediated physiology and pathology as well as a potential drug candidate for leukemia and other cancers.
• In Vitro:
  A highly selective inhibitor compound 40 (JSH-150), which exhibited an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieved around 300 10000-fold selectivity over other CDK kinase family members. In addition, it also displayed high selectivity over other 468 kinases/mutants (KINOMEscan S score(1) = 0.01).Compound 40 displayed potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines. It could dose-dependently inhibit the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrest the cell cycle and induce the apoptosis in the leukemia cells.

Storage & Handling

• Storage: keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK9, CDK, Cyclin dependent kinase, Inhibitor, inhibit, JSH 150, JSH150, JSH-150

Compound Identifiers

PubChem CID

134814484